Transdermal dosage form comprising an active agent and a salt and a free-base form of an adverse agent

Abstract

This invention relates to a tamper-resistant transdermal dosage form comprising an active agent, such as an opioid, or a pharmaceutically acceptable salt thereof, a free base of an adverse agent, such as an opioid antagonist, and a pharmaceutically acceptable salt of an adverse agent, such as an opioid antagonist. The transdermal dosage form allows an effective amount of the active agent, or a pharmaceutically acceptable salt thereof, to be transdermally administered to an animal. The invention further relates to methods for treating or preventing pain in an animal comprising contacting the skin of an animal in need thereof with the transdermal dosage form of the invention for an amount of time sufficient to treat or prevent pain.

Description

1. FIELD OF THE INVENTION [0001] The present invention relates to transdermal dosage forms useful for preventing or discouraging the abuse of an active pharmaceutical agent, such as an opioid. The present invention further relates to tamper-resistant transdermal dosage forms comprising an active pharmaceutical agent or a pharmaceutically acceptable salt thereof, and an adverse agent of the active pharmaceutical agent, the adverse agent comprising both a free base adverse agent and a pharmaceutically acceptable salt of the adverse agent. In particular, the present invention relates to tamper-resistant transdermal dosage forms comprising an opioid or a pharmaceutically acceptable salt thereof, a free-base opioid antagonist, and a pharmaceutically acceptable salt of an opioid antagonist. 2. BACKGROUND OF THE INVENTION [0002] Transdermal dosage forms are convenient for delivering many different therapeutically effective agents, including but not limited to analgesics, such as opioid ana...

AI Technical Summary

Benefits of technology

[0011] In another embodiment, the present invention is directed to transdermal dosage forms comprising an active agent, a pharmaceutically acceptable salt of an adverse agent and an adverse agent in the form of a free base, in an amount sufficient to inhibit at least one biological effect of the active agent.

[0012] In another embodiment, the present invention is directed to a transdermal dosage form comprising an analgesically effective amount of an opioid or a pharmaceutically acceptable salt thereof (hereinafter “Opioid”), an opioid antagonist in the form of a free base (hereinafter “Antagonist Free Base”),

Problems solved by technology

However, many dosage forms, and particularly those intended for timed and sustained release of active agents, contain large amounts of active agents, often in an amount that is many times the actual dose absorbed or delivered.

Thus, there is often a significant amount of the active agent remaining in the dosage form after use and removal of the device by the user.

Both the unused dosage form and the portion of active agent that remains in the dosage form after use are potentially subject to intentional or inadvertent abuse or misuse, particularly if the active agent is a narcotic or a controlled substance.

Even careful disposal of used dosage forms might not be completely effective for preventing abuse, particularly in cases of incomplete or partial compliance.

The patent does not address the problem of abuse of the active drug, and does not address the use of antagonists to prevent such abuse.

The patent does not address the problem of extraction using different solvent systems, and does not disclose the use of multiple antagonists having differing solubilities.

The inadvertent misuse or abuse of transdermal dosage forms remains a significant health problem.

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